- Synthesis, Antimicrobial Activity and Molecular Modeling of Some Novel 5-Aminopyrazole, Pyrazolo[1,5-a]pyrimidine, Bispyrazole and Bispyridone Derivatives Containing Antipyrinyl Moiety
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2-Cyano-N-(antipyrin-4-yl)-3-(ethylthio)-3-(naphthalen-1-ylamino)acryl-amide 4 was achieved via a one-pot, three-component reactions of cyanoacetamide derivative 2, 2-naphthyl isothiocyanate, and diethyl-sulphate. The cyano acrylamide derivative 4 was hydrazinolysis to furnish 5-aminopyrazole 5; many pyrazolo[1,5-a]pyrimidines 10a,b, 14, 15, 16, 18, and 20 have been synthesized via treatment of 5 with some electrophilic reagents. Also, ternary condensation of cyanoacetamide derivative 2, terephthalaldehyde, and active methylene derivatives afforded bispyridone derivatives 21a,b. The structures of the new compounds were confirmed on the basis of elemental analysis and spectral data. Representative compounds of the synthesized products were tested and evaluated as antimicrobial. In general, the novel-synthesized compounds showed a good antimicrobial activity against Gram-positive bacteria, Gram-negative bacteria, and antifungal activity against Azithromycin and Ketoconazole. The molecular modeling of the 21a and 21b as representative examples of the synthesized compounds has been drawn, and their molecular parameters were calculated.
- Helal, Mohamed Hamdy,Salem, Mohamed A.,Aly, Hala Mohamed
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- Synthesis and anti-hbv activity of 4-aminoanti- pyrine derivatives
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The reactions of 4-aminoantipyrine with acetylacetone, ethyl acetoacetate, morpholine, piperazine, and ethyl cyanoacetate were studied. All structures were determined by 1H NMR and mass spectroscopy techniques.
- Abdel-Rahman,Ahmed,Ramiz
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experimental part
p. 72 - 78
(2010/08/05)
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- Design and synthesis of some thiazolyl and thiadiazolyl derivatives of antipyrine as potential non-acidic anti-inflammatory, analgesic and antimicrobial agents
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The synthesis of two groups of structure hybrids comprising basically the antipyrine moiety attached to either polysubstituted thiazole or 2,5-disubstituted-1,3,4-thiadiazole counterparts through various linkages is described. Twelve out of the newly synt
- Rostom, Sherif A.F.,El-Ashmawy, Ibrahim M.,Abd El Razik, Heba A.,Badr, Mona H.,Ashour, Hayam M.A.
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scheme or table
p. 882 - 895
(2009/08/15)
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- A convenient route to pyridones, pyrazolo[2,3-a]pyrimidines and pyrazolo[5,1-c]triazines incorporating antipyrine moiety
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Condensation of 4-aminoantipyrine with ethyl acetoacetate, ethyl benzoylacetate, and ethyl cyanoacetate furnished the corresponding ethyl 3-(1,2-dihydro-1,5-dimethyl-2-phenyl-3-oxo-3H-pyrazol-4-yl)aminoacrylate and 2-cyano-N-[(1,2-dihydro-1,5-dimethyl-2-p
- Farag, Ahmad M.,Dawood, Kamal M.,Elmenoufy, Hanan A.
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p. 508 - 514
(2007/10/03)
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